CN107957381A - A kind of assay method of spirolactone Dissolution of Tablet - Google Patents
A kind of assay method of spirolactone Dissolution of Tablet Download PDFInfo
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- CN107957381A CN107957381A CN201711326299.XA CN201711326299A CN107957381A CN 107957381 A CN107957381 A CN 107957381A CN 201711326299 A CN201711326299 A CN 201711326299A CN 107957381 A CN107957381 A CN 107957381A
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N13/00—Investigating surface or boundary effects, e.g. wetting power; Investigating diffusion effects; Analysing materials by determining surface, boundary, or diffusion effects
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Abstract
The present invention relates to a kind of assay method of pharmaceutical solid preparation dissolution in vitro, more particularly to a kind of assay method of spirolactone Dissolution of Tablet, the method, step is as follows：Step 1,15L dissolution mediums are prepared, take that spirolactone copies piece and original grinds each 12 of piece respectively, in the intelligent digestion instrument of 12 glasss of input, method to set up：Slurry processes 75r/min, 1000ml are dissolution volume, and sample point is respectively 10min, 15min, 20min, 30min, 45min, 60min, 90min, 120min.Step 2, sampled respectively at above-mentioned sample point and carry out spirolactone stripping quantity measure, compare the stripping quantity of two kinds of each sample points of tablet, calculate the f2 factors.
Description
Technical field
The present invention relates to a kind of assay method of pharmaceutical solid preparation dissolution in vitro, more particularly to a kind of spirolactone tablet
The assay method of dissolution rate.
Background technology
Spirolactone.Chemical name：17 beta-hydroxy-3- oxygen pregnant steroid-4 of-7a- (acetylthio)-17a--alkene-21-carboxylic acids
Y-lactone.Primary efficacy is：
(1) edema disease is shared with other diuretics, treats the water such as congested oedema, cirrhotic ascites, renal edema
Swollen property disease, the secondary aldosterone secretion that its object is to correct above-mentioned disease when occurs together increases, and resists other diuretics
Row's potassium effect.It is also used for the treatment of idiopathic edema.
(2) ancillary drug of the hypertension as treatment hypertension.
(3) primary aldosteronism spirolactone can be used for this sick diagnose and treat.
(4) prevention of hypopotassaemia is shared with thiazide diuretic, enhancing diuresis effect and prevention hypopotassaemia.
Spirolactone tablet is the main spirolactone preparation that has listed, it is necessary to often detect its dissolution rate, existing dissolution rate
Assay method mainly use using the 0.1mol/L hydrochloric acid solutions 1000ml of 0.1% lauryl sodium sulfate as dissolution medium evaluate
In Vitro Dissolution, dissolution sample point are 60min, and limit is the 80% of labelled amount；The method does not investigate different sample points and other pH
Dissolution medium in In Vitro Dissolution situation, it is impossible to reaction self-control medicine and the former dissolved corrosion for grinding vitro Drug completely.
At present the Spironolactone Tablets that have listed due on prescription and technique with former triturate there are bigger difference, may reach not
The effect of medicine is consistent is ground to original.Need to carry out Conformance Assessment for this, the present invention is coordinates Conformance Assessment, on
The imitated pharmaceutical preparation in city grinds whether the behavior of pharmaceutical preparation In Vitro Dissolution unanimously provides a kind of detection method with original, as imitation medicine
Thing and the original reference index that to grind curative effect of medication consistent.
The content of the invention
A kind of detection method of Spironolactone Tablets dissolution rate of present invention offer, the method, step are as follows：Step 1, prepare
15L dissolution mediums, take that spirolactone copies piece and original grinds each 12 of piece respectively, in the intelligent digestion instrument of 12 glasss of input, method to set up：
Slurry processes 75r/min, 1000ml are dissolution volume, sample point be respectively 10min, 15min, 20min, 30min, 45min, 60min,
90min、120min。
Step 2, sampled respectively at above-mentioned sample point and carry out spirolactone stripping quantity measure, compare two kinds of each sample points of tablet
Stripping quantity, calculate the f2 factors.
Wherein, the dissolution medium, is selected from：+ 1.0% Tween 80 of pH4.5 acetate buffers, pH6.8 phosphate-buffereds
The Tween 80 of liquid+1.0%, three kinds of the Tween 80 of water+1.0%.
With the detection method of the present invention, it can really reflect the dissolution rates of the Spironolactone Tablets of two kinds of separate sources.
The difference of the method and existing method of the present invention is further illustrated below by way of experiment：
It was found from data above, the method for the embodiment of the present invention 1 is better than the prior art on many index.
In Vitro Dissolution measure is carried out to self-control preparation and reference preparation as dissolution medium, with evaluation self-control preparation and reference
Whether agent in vitro dissolution is consistent.
To grind medicine difference larger due to prescription and original for the Spironolactone Tablets of country's listing, causes only dissolution determination qualification,
But stripping curve grinds that medicine gap is larger with original, implement such scheme and can eliminate to grind the inconsistent imitation medicine of medicine with former, and
Index is provided for newly imitated medicine.
Embodiment：
The present invention is further illustrated by the following examples.
Embodiment 1
The preparation of+1.0% Tween 80 medium of pH4.5 acetate buffers：Tween 80 10g is weighed, takes anhydrous sodium acetate
1.8g, adds water 1L, adds glacial acetic acid 1.6ml, shakes up, and ultrasound makes dissolving, degassing, to obtain the final product.
Above-mentioned medium prepares 15L, is taken respectively from preparation and reference preparation 12, puts into 12 glasss of intelligent digestion instrument,
Method to set up：Slurry processes 75r/min, 1000ml are dissolution volume, sample point be respectively 10min, 15min, 20min, 30min,
45min、60min、90min、120min.It is measured respectively at the sampling of above-mentioned sample point, compares self-control preparation and reference preparation
The stripping quantity of each sample point, calculates the f2 factors.
As a result it is as follows：
| 10min | 15min | 20min | 30min | 45min | 60min | 90min | 120min | |
| Reference preparation | 27 | 52 | 67 | 79 | 85 | 88 | 90 | 92 |
| Make preparation by oneself | 16 | 48 | 63 | 73 | 88 | 92 | 95 | 98 |
Embodiment 2
The preparation of+1.0% Tween 80 medium of pH6.8 phosphate buffers：Tween 80 10g is weighed, takes potassium dihydrogen phosphate
6.8g, takes sodium hydroxide 0.9g, adds water 1L, shakes up, and ultrasound makes dissolving, degassing, to obtain the final product.
Above-mentioned medium prepares 15L, is taken respectively from preparation and reference preparation 12, puts into 12 glasss of intelligent digestion instrument,
Method to set up：Slurry processes 75r/min, 1000ml are dissolution volume, sample point be respectively 10min, 15min, 20min, 30min,
45min、60min、90min、120min.It is measured respectively at the sampling of above-mentioned sample point, compares self-control preparation and reference preparation
The stripping quantity of each sample point, calculates the f2 factors.
As a result it is as follows
| 10min | 15min | 20min | 30min | 45min | 60min | 90min | 120min | |
| Reference preparation | 13 | 27 | 41 | 53 | 59 | 62 | 63 | 65 |
| Make preparation by oneself | 16 | 35 | 43 | 51 | 59 | 72 | 80 | 82 |
Embodiment 3
The preparation of the Tween 80 medium of water+1.0%：Tween 80 10g is weighed, adds water 1L, shakes up, ultrasound makes dissolving, degassing,
To obtain the final product.
Above-mentioned medium prepares 15L, is taken respectively from preparation and reference preparation 12, puts into 12 glasss of intelligent digestion instrument,
Method to set up：Slurry processes 75r/min, 1000ml are dissolution volume, sample point be respectively 10min, 15min, 20min, 30min,
45min、60min、90min、120min.It is measured respectively at the sampling of above-mentioned sample point, compares self-control preparation and reference preparation
The stripping quantity of each sample point, calculates the f2 factors.
As a result it is as follows：
| 10min | 15min | 20min | 30min | 45min | 60min | 90min | 120min | |
| Reference preparation | 13 | 35 | 55 | 72 | 81 | 85 | 88 | 92 |
| Make preparation by oneself | 17 | 41 | 54 | 68 | 83 | 90 | 96 | 98 |
The screening of dissolution medium of the present invention, screening process are as follows：
Reference《Imitation medicine quality and curative effect Conformance Assessment regulation》And version in 2015《Chinese Pharmacopoeia》The system of dissolution medium
Preparation Method, outside desalination acid solution, the medium of other pH is the pH4.5 acetate buffers in regulation, pH6.8 phosphate-buffereds
Liquid, and water.Since spirolactone is insoluble drug, water is practically insoluble in, therefore when evaluating the medium of In Vitro Dissolution, it should add suitable
The surfactant of amount, since lauryl sodium sulfate can react with the auxiliary material calcium sulfate in reference preparation, therefore selection is spat
Temperature 80 is used as surfactant, screen be separately added under each medium 0.2% Tween 80,0.5% Tween 80,0.8% Tween 80,
The dissolving situation of bulk pharmaceutical chemicals, result of the test show during 1.0% Tween 80：When above-mentioned medium adds 1.0% Tween 80, dissolubility compared with
It is good, and according to《Normal oral solid pharmaceutical preparation stripping curve measure guideline compared with》, it is proposed that add surfactant concentration
Recommend in 0.01%-1.0% (W/V) scope, therefore filter out surfactant concentration as 1.0%.
Filter out with+1.0% Tween 80 of pH4.5 acetate buffers ,+1.0% Tween 80 of pH6.8 phosphate buffers,
The Tween 80 of water+1.0% is dissolution medium, and carrying out In Vitro Dissolution to Spironolactone Tablets is instructed and evaluated.By dissolution medium
Screening, filter out with+1.0% Tween 80 of pH4.5 acetate buffers ,+1.0% Tween 80 of pH6.8 phosphate buffers, water+
1.0% Tween 80 is dissolution medium, and carrying out In Vitro Dissolution to Spironolactone Tablets is instructed and evaluated.
Claims (2)
1. a kind of assay method of spirolactone Dissolution of Tablet, the method, step are as follows：
Step 1,15L dissolution mediums are prepared, take that spirolactone copies piece and original grinds each 12 of piece, the intelligent dissolution of 12 glasss of input respectively
In instrument, method to set up：Slurry processes 75r/min, 1000ml are dissolution volume, sample point be respectively 10min, 15min, 20min,
30min, 45min, 60min, 90min, 120min,
Step 2, sampled respectively at above-mentioned sample point and carry out spirolactone stripping quantity measure, compare the molten of two kinds of each sample points of tablet
Output, calculates the f2 factors.
2. according to the method described in claim 1, wherein, the dissolution medium, is selected from：PH4.5 acetate buffers+1.0%
Tween 80 ,+1.0% Tween 80 of pH6.8 phosphate buffers, three kinds of the Tween 80 of water+1.0%.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111089821A (en) * | 2018-10-23 | 2020-05-01 | 武汉武药科技有限公司 | Dissolution rate determination method and application of eltrombopag tablets |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106018604A (en) * | 2016-05-25 | 2016-10-12 | 中山大学 | Method for measuring dissolution rates of esomeprazole magnesium enteric-coated preparation in different media |
| CN106645481A (en) * | 2016-12-23 | 2017-05-10 | 东药集团沈阳施德药业有限公司 | Method for testing dissolution curve of quick release dosage form drug-amoxicillin and clavulanate potassium dispersible tablet |
-
2017
- 2017-12-13 CN CN201711326299.XA patent/CN107957381A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106018604A (en) * | 2016-05-25 | 2016-10-12 | 中山大学 | Method for measuring dissolution rates of esomeprazole magnesium enteric-coated preparation in different media |
| CN106645481A (en) * | 2016-12-23 | 2017-05-10 | 东药集团沈阳施德药业有限公司 | Method for testing dissolution curve of quick release dosage form drug-amoxicillin and clavulanate potassium dispersible tablet |
Non-Patent Citations (5)
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| 张强等: "《药剂学》", 31 January 2005 * |
| 张翔等: "吲达帕胺片仿制药与原研药的溶出度一致性评价", 《中国药物警戒》 * |
| 徐斌等: "坎地沙坦酯氨氯地平片的溶出度测定", 《药学研究》 * |
| 曾钰等: "螺内酯片的溶出度测定与质量分析", 《中国医院药学杂志》 * |
| 牛华英等: "硝苯地平制剂的溶出度测定方法", 《齐鲁药事》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111089821A (en) * | 2018-10-23 | 2020-05-01 | 武汉武药科技有限公司 | Dissolution rate determination method and application of eltrombopag tablets |
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Application publication date: 20180424 |